Potent and Orally Bioavailable Non-Peptide Antagonists at the Human Bradykinin B1 Receptor Based on a 2-Alkylamino-5-sulfamoylbenzamide Core
- 10 August 2004
- journal article
- letter
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 47 (19) , 4642-4644
- https://doi.org/10.1021/jm049747g
Abstract
The bradykinin B(1) receptor is rapidly induced after inflammation or tissue trauma and appears to play an important role in the maintenance of hyperalgesia in inflammatory conditions. Here, we describe the optimization process to identify novel, potent non-peptide human B(1) receptor antagonists based on a 2-alkylamino-5-sulfamoylbenzamide core. Optimized derivatives are selective, functional B(1) antagonists with low nanomolar affinity and exhibit oral bioavailability in animals.Keywords
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